Design and Evaluation of Bilayer Pump Tablet of Flurbiprofen Solid Dispersion for Zero-Order Controlled Delivery

Cheng, Lizhen; Li, Ting; Dong, Ling; Wang, Xiaoyu; Huo, Qiye; Wang, Haoyu; Jiang, Zhujun; Shan, Xinyu; Pan, Weisan; Yang, Xinggang

doi:10.1016/j.xphs.2017.12.026

Cited by 15 publications

(6 citation statements)

References 25 publications

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“…This biphasic release pattern is an important parameter responsible to extend the drug release. The SEM analysis of tablet dissolution showed that the significant porosity during the dissolution is the result of the leaching of water-soluble additives during dissolution [38]. The multiple parameters like weight gain (coating), agitation speed, orifice diameter, coating membrane thickness pH of media showed negligible effect on drug release [39][40][41][42][43][44].…”

Section: Discussionmentioning

confidence: 99%

Development, optimization and pharmacokinetic evaluation of biphasic extended-release osmotic drug delivery system of trospium chloride for promising application in treatment of overactive bladder

Gundu

Pekamwar

Shelke³

et al. 2021

Futur J Pharm Sci

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Background The research was aimed with an approach to formulate biphasic extended-release system of trospium chloride resulting in controlled release of drug up to 24 h with prospects of better control on urinary frequency, efficacy, tolerability, and improved patient compliance. The push–pull osmotic pump (PPOP) bi-layered tablet of trospium chloride (60 mg) was developed with the use of immediate-release polymers in the pull layer (30 mg drug) and polyethylene oxide in the push layer (remaining 30 mg drug). The tablet was formulated by compression after non-aqueous granulation, seal coating, and semipermeable coating. The tablet prepared was laser drilled to create an orifice for drug release. Results Comparative in vitro dissolution and in vivo pharmacokinetic analysis of available marketed formulations demonstrated the complete drug release within 16–18 h; hence the developed biphasic extended-release system has its great importance as it provides zero-order release up to 24 h. Conclusions The developed biphasic extended-release drug delivery system of trospium chloride provides the drug release for 24 h with effective plasma concentration in comparison with the available marketed formulation. Extended release of drug from the developed formulation provides scope for its promising application in the treatment of overactive bladder (OAB).

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Section: Discussionmentioning

confidence: 99%

Development, optimization and pharmacokinetic evaluation of biphasic extended-release osmotic drug delivery system of trospium chloride for promising application in treatment of overactive bladder

Gundu

Pekamwar

Shelke³

et al. 2021

Futur J Pharm Sci

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“…The heat exposure during the preparation and analysis of the eutectic mixtures was not expected to cause any drug degradation of the two rather stable compounds, in line with previous reports that employed hot melt extrusion. 22,23 The obtained molten mixture in the present work was then cooled to room temperature and kept in a desiccator before analysis. Characteristics and compositions for various drug−PEG eutectic systems are described in Table 1.…”

Section: ■ Materials and Methodsmentioning

confidence: 99%

Broadband Diffusing Wave Spectroscopy Reveals Microstructuring of Polymer–Drug System

Jankovic

Aleandri

Reufer³

et al. 2020

Crystal Growth & Design

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Microstructuring during a phase transition and crystallization, in particular, is critical for the physicochemical properties of polymeric drug carriers and of the final dosage form. Extensive research has been dedicated to studying polymeric matrices in drug delivery, and despite substantial progress, there are still unmet challenges such as noninvasive mechanical analysis because classical rheological methods typically disturb the samples, in particular, during a phase transition. This article employs diffusing wave spectroscopy (DWS) over a broad frequency band to study polymer−drug systems in a noninvasive way. Eutectic mixtures of polyethylene glycol were investigated using two model drugs. Whereas fenofibrate barely interacted with the polymer, flurbiprofen provided a compound showing distinct molecular interactions with the carrier. Mechanical spectra were obtained during cooling of the molten polymer−drug systems. In conclusion, broadband DWS provided a better mechanistic understanding of the polymer−drug interactions and of macromolecular structuring during cooling of the eutectic melts. Such findings are relevant for a rationale design of pharmaceutical formulations during development, and such knowledge would be also important for manufacturing to achieve drug products with reproducible quality characteristics.

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“…The bilayer tablets were prepared by doublecompressing procedure with a lab tablet press (DP30A, Longli Tech, Beijing, China) (21,22). A fixed dose of the granules of IBU layer was loaded into the die cavity and precompressed manually, and then the powder of PE layer was filled and compressed to be a bilayer tablet.…”

Section: Preparation Of the Sustained Release Bilayer Tabletsmentioning

confidence: 99%

Sustained Release Bilayer Tablet of Ibuprofen and Phenylephrine Hydrochloride: Preparation and Pharmacokinetics in Beagle Dogs

Zhu

Han

et al. 2019

AAPS PharmSciTech

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Cold is a global common infectious disease accompanied by symptoms such as headache and stuffy nose. Ibuprofen (IBU) and phenylephrine hydrochloride (PE) were commonly used for common cold due to their different effects in relieving fever and the main symptoms such as nasal congestion and high sinus pressure. However, the commercial tablets of IBU and PE have to be administered 2 to 3 times per day due to their short half-life, with inconvenience for patient and fluctuations of plasma concentration. Bilayer tablet technology was utilized to design the IBU-PE sustained release tablets because of the significantly different solubility of IBU and PE in release media. The formulations of IBU layer and PE layer contain different viscosity grades of hydroxypropyl methylcellulose (HPMC) as sustained-release matrix, hydrophilic diluent, and traditional glidant and lubricant. The sustained release bilayer tablet exhibited satisfying sustained release performance with the mechanisms of diffusion and matrix erosion. Compared with the conventional tablets, the IBU-PE sustained release bilayer tablet expressed significantly sustained-release behavior with decreased C max and prolonged T max in fasted conditions for IBU and PE. Though IBU of IBU-PE sustained release bilayer tablet was bioequivalent to the commercial IBU tablet, the relative bioavailability of PE from the bilayer tablets was 87.49 ± 20.00% (90% confidence interval was 72.3 to 102.5%), indicating bioinequivalence probably due to the Bfirst pass^effect.

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Design and Evaluation of Bilayer Pump Tablet of Flurbiprofen Solid Dispersion for Zero-Order Controlled Delivery

Cited by 15 publications

References 25 publications

Development, optimization and pharmacokinetic evaluation of biphasic extended-release osmotic drug delivery system of trospium chloride for promising application in treatment of overactive bladder

Development, optimization and pharmacokinetic evaluation of biphasic extended-release osmotic drug delivery system of trospium chloride for promising application in treatment of overactive bladder

Broadband Diffusing Wave Spectroscopy Reveals Microstructuring of Polymer–Drug System

Sustained Release Bilayer Tablet of Ibuprofen and Phenylephrine Hydrochloride: Preparation and Pharmacokinetics in Beagle Dogs

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